General Information of Drug Therapeutic Target (DTT) (ID: TTDEQIP)

DTT Name Pyruvate dehydrogenase kinase 3 (PDHK3)
Synonyms Pyruvate dehydrogenase kinase isoform 3; PDK3
Gene Name PDK3
DTT Type
Literature-reported target
[1]
BioChemical Class
Kinase
UniProt ID
PDK3_HUMAN
TTD ID
T99029
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 2.7.11.2
Sequence
MRLFRWLLKQPVPKQIERYSRFSPSPLSIKQFLDFGRDNACEKTSYMFLRKELPVRLANT
MREVNLLPDNLLNRPSVGLVQSWYMQSFLELLEYENKSPEDPQVLDNFLQVLIKVRNRHN
DVVPTMAQGVIEYKEKFGFDPFISTNIQYFLDRFYTNRISFRMLINQHTLLFGGDTNPVH
PKHIGSIDPTCNVADVVKDAYETAKMLCEQYYLVAPELEVEEFNAKAPDKPIQVVYVPSH
LFHMLFELFKNSMRATVELYEDRKEGYPAVKTLVTLGKEDLSIKISDLGGGVPLRKIDRL
FNYMYSTAPRPSLEPTRAAPLAGFGYGLPISRLYARYFQGDLKLYSMEGVGTDAVIYLKA
LSSESFERLPVFNKSAWRHYKTTPEADDWSNPSSEPRDASKYKAKQ
Function
Inhibits pyruvatedehydrogenase activity by phosphorylation of the E1 subunit PDHA1, and thereby regulates glucose metabolism and aerobic respiration. Can also phosphorylate PDHA2. Decreases glucose utilization and increases fat metabolism in response to prolonged fasting, and as adaptation to a high-fat diet. Plays a role in glucose homeostasis and in maintaining normal blood glucose levels in function of nutrient levels and under starvation. Plays a role in the generation of reactive oxygen species.
KEGG Pathway
Diabetic cardiomyopathy (hsa05415 )
Reactome Pathway
Signaling by Retinoic Acid (R-HSA-5362517 )
Regulation of pyruvate dehydrogenase (PDH) complex (R-HSA-204174 )

References

1 Inactivation of the HIF-1/PDK3 signaling axis drives melanoma toward mitochondrial oxidative metabolism and potentiates the therapeutic activity o... Cancer Res. 2012 Oct 1;72(19):5035-47.